A large number of antibiotics are used therapeutically for treating infectious bacterial diseases. However, the pathogens are becoming increasingly resistant to the pharmaceuticals employed, and there is even the threat of a serious risk due to what are termed multiresistant organisms, which have not only become capable of resisting single antibiotic groups, such as β-lactam antibiotics, glycopeptides or macrolides, but also carry several resistances at one and the same time. There are even pathogens which have become resistant to all the commercially available antibiotics. Infectious diseases that are caused by these organisms can no longer be treated. There is, therefore, a great need for novel agents which can be used against resistant organisms. While thousands of antibiotics have been described in the literature, most of them are too toxic to be used as pharmaceuticals.
A relatively large number of polyene antibiotics, most of which are macrolides, that is their structures belong to the macrocyclic structure type, have already been described. These macrolides act antimycotically by means of interactions with biological membranes, and are, therefore, toxic to warm-blooded animals (homeotherms). The most important representative of this antibiotic type is amphotericin B, which is used as a therapeutic agent in humans despite its toxicity. An example of a nonmacrocyclic polyene antibiotic which has been described (Ritzau et al., Liebigs Ann. Chem. 1993, 433-435) is serpentene, which contains a phenyl ring which is substituted in the 1,2 position by polyene side chains. In tests directed against Gram-positive and Gram-negative bacteria, serpentene only exhibited a weak antibiotic effect against Bacillus subtilis. 
The cell wall of Gram-positive bacteria is composed, inter alia, of murein, which is composed of N-acetyl-D-glucosamine and N-acetylmuramic acid, which are linked to each other like a disaccharide, and contains amino acids and peptides, such as D-glutamine, D- and L-alanine, L-lysine and pentaglycyl units, and which is strongly cross-linked. The biosynthesis of the bacterial cell wall takes place using enzymes which are not found in homeotherm metabolism. These enzymes are, therefore, suitable sites of attack for developing antibiotics which are well tolerated by homeotherms. Furthermore, inhibitors of murein biosynthesis should not be poisonous to humans. Glycosyltransferase (Transglycosylase, GT) is a key enzyme in peptidoglycan biosynthesis and, consequently, of cell wall construction. A specific inhibitor of this enzyme, i.e. moenomycin (Kurz et al., Eur. J. Biochem. 1998, 252, 500-507), has been known for a relatively long time. Moenomycin is an antibiotic which exhibits very powerful activity and which is well tolerated; however, it is not absorbed from the gastrointestinal tract, and elimination from the blood following intravenous administration is also difficult. For these reasons, it has thus far not been possible to use moenomycin systemically in medicine. Further, only a very few additional glycosyltransferase inhibitors have been described in the literature; for reasons of pharmacokinetics or tolerance, none of these agents has found its way into therapy. For this reason, novel GT inhibitors are still being sought, as has recently been reported by Goldman & Gange in Current Medicinal Chem. 2000, 7, 801-820. Screening for GT inhibitors employs specific biochemical GT test systems; such assays have been described repeatedly, for example, by Vollmer & Höltje in Antimicrobial Agents and Chemotherapy 2000, 44, 1181-1185.
Darby et al. (J. Org. Chem. 1977, 42, 1960-1967) describe the synthesis of phenyl compounds which are substituted by trans-polyene side chains in the 1,2 position for analyzing the π system of macrocyclic annulenes.